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    • 2. 发明公开
    • 벤자스타틴 유도체의 제조시 중간체로 사용 가능한 새로운화합물 및 그 제조방법
    • 作为制备苯扎他汀衍生物的中间体的新化合物及其制备方法
    • KR1020020018100A
    • 2002-03-07
    • KR1020010052436
    • 2001-08-29
    • 주식회사한국신약
    • 유익동홍남두조원제이찬복김진표김원곤
    • C07D209/24
    • PURPOSE: Provided is a novel compound useful as an intermediate in manufacturing benzastatin derivatives having an excellent inhibition activity of lipid peroxidation. Also, its manufacturing method is provided. CONSTITUTION: The novel compound is a basic structure of benzastatin useful as an inhibitor of lipid peroxidation and represented by the formula(1), wherein R1 is H, CH3, OH, nitrile group, amide group, C1-C4 alkoxy group or hydroxymethyl group; R2 is a nitrogen protection group, such as H, CH3 or PMB(paramethoxy benzyl); and R3 is H, CH3, C1-C10 alkyl group or partially unsaturated linear or branched hydrocarbon. Aldehyde compound of the formula(1a) is manufactured by the steps of: reducing a compound of the formula(5) with a reductant to prepare a compound of the formula(6); and oxidizing the alcohol compound of the formula(6) to obtain a compound of the formula(1a).
    • 目的:提供一种在制备具有优异的脂质过氧化抑制活性的苯达斯汀衍生物中作为中间体的新型化合物。 此外,还提供了其制造方法。 构成:新化合物是用作脂质过氧化抑制剂的苯达斯汀的基本结构,由式(1)表示,其中R1是H,CH3,OH,腈基,酰胺基,C1-C4烷氧基或羟甲基 ; R2是氮保护基团,例如H,CH 3或PMB(对甲氧基苄基); 并且R 3是H,CH 3,C 1 -C 10烷基或部分不饱和直链或支链烃。 通过以下步骤制备式(1a)的醛化合物:用还原剂还原式(5)的化合物以制备式(6)的化合物; 氧化式(6)的醇化合物,得到式(1a)的化合物。
    • 7. 发明公开
    • 카페오일 퀴닉산 유도체, 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 주름 개선용 조성물
    • 含有CAFFEOYLQUINIC酸衍生物的抗皱组合物,作为活性成分的药物可接受的盐
    • KR1020110043195A
    • 2011-04-27
    • KR1020090100207
    • 2009-10-21
    • 주식회사한국신약
    • 유익동허광화유재국한상욱
    • A61K31/192A61P17/18A61K31/216A61K8/36
    • PURPOSE: A composition containing caffeoyl quinic acid derivatives and pharmaceutically acceptable salt thereof is provided to effectively suppress elastase activity of human neutrophil and to ensure anti-wrinkling. CONSTITUTION: A composition contains caffeoyl quinic acid derivatives and pharmaceutically acceptable salt thereof as an active ingredient. The composition is derived from one selected from the group consisting of (1S,3R,4R,5R)-3,4-bis((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)-1,5 dihydroxycyclohexane carboxylic acid, (1S,3R,4R,5R)-methyl-3,4-bis((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)-1,5-dihydroxycyclohexanecarboxylate, (1R,3R,4S,5R)-methyl-4,5-bis((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)-1,5-dihydroxycyclohexanecarboxylate, (1S,3R,4S,5R)-3,5-bis((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)-1,4-dihydroxycyclohexanecarboxylic acid, and (1S,3R,4S,5R)-methyl-3,5-bis((E)-3-(3,4-dihydroxyphenyl)acryloyloxy)-1,4-dihydroxycyclohexanecarboxylate.
    • 目的:提供含有咖啡酰奎尼酸衍生物及其药学上可接受的盐的组合物,以有效抑制人嗜中性粒细胞的弹性蛋白酶活性并确保抗皱纹。 构成:组合物含有咖啡酰奎尼酸衍生物及其药学上可接受的盐作为活性成分。 该组合物衍生自选自(1S,3R,4R,5R)-3,4-双((E)-3-(3,4-二羟基苯基)丙烯酰氧基)-1,5-二羟基环己烷羧酸 ,(1S,3R,4R,5R) - 甲基-3,4-二((E)-3-(3,4-二羟基苯基)丙烯酰氧基)-1,5-二羟基环己烷羧酸酯,(1R,3R,4S,5R) ((E)-3-(3,4-二羟基苯基)丙烯酰氧基)-1,5-二羟基环己烷羧酸酯,(1S,3R,4S,5R)-3,5-双((E) -3-(3,4-二羟基苯基)丙烯酰氧基)-1,4-二羟基环己烷羧酸和(1S,3R,4S,5R) - 甲基-3,5-双((E) 二羟基苯基)丙烯酰氧基)-1,4- dihydroxycyclohexanecarboxylate。